WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H525580
CAS#: 163059-33-4
Description: LY-368975 is a potent and selective inhibitor of the norepinephrine (NE) reuptake site. It is capable of reducing food consumption in rodents. Compounds of this class may have use in the treatment of obesity and eating disorders.
Hodoodo Cat#: H525580
Name: LY-368975
CAS#: 163059-33-4
Chemical Formula: C17H21NOS
Exact Mass: 287.13
Molecular Weight: 287.420
Elemental Analysis: C, 71.04; H, 7.36; N, 4.87; O, 5.57; S, 11.15
This product is not in stock, which may be available by custom synthesis.
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Synonym: LY-368975; LY 368975; LY368975; (R)-Thionisoxetine.
IUPAC/Chemical Name: Benzenepropanamine, N-methyl-gamma-(2-(methylthio)phenoxy)-, (gammaR)-
InChi Key: NDVZIUGCCMZHLG-HNNXBMFYSA-N
InChi Code: InChI=1S/C17H21NOS/c1-18-13-12-15(14-8-4-3-5-9-14)19-16-10-6-7-11-17(16)20-2/h3-11,15,18H,12-13H2,1-2H3/t15-/m0/s1
SMILES Code: CNCC[C@@H](c1ccccc1)Oc2ccccc2SC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 287.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Filannino MA, Matarrese M, Turolla EA, Masiello V, Moresco RM, Todde S, Verza E, Magni F, Cattaneo A, Bachi A, Kienle MG, Fazio F. Synthesis and carbon-11 labeling of (R)- and (S)-thionisoxetine, norepinephrine reuptake inhibitors, potential radioligands for positron emission tomography. Appl Radiat Isot. 2007 Nov;65(11):1232-9. Epub 2007 Jun 26. PubMed PMID: 17646106.
2: Jones CK, Eastwood BJ, Need AB, Shannon HE. Analgesic effects of serotonergic, noradrenergic or dual reuptake inhibitors in the carrageenan test in rats: evidence for synergism between serotonergic and noradrenergic reuptake inhibition. Neuropharmacology. 2006 Dec;51(7-8):1172-80. Epub 2006 Oct 11. PubMed PMID: 17045620.
3: Iyengar S, Webster AA, Hemrick-Luecke SK, Xu JY, Simmons RM. Efficacy of duloxetine, a potent and balanced serotonin-norepinephrine reuptake inhibitor in persistent pain models in rats. J Pharmacol Exp Ther. 2004 Nov;311(2):576-84. Epub 2004 Jul 13. PubMed PMID: 15254142.
4: Katofiasc MA, Nissen J, Audia JE, Thor KB. Comparison of the effects of serotonin selective, norepinephrine selective, and dual serotonin and norepinephrine reuptake inhibitors on lower urinary tract function in cats. Life Sci. 2002 Aug 2;71(11):1227-36. PubMed PMID: 12106588.
5: Rowland NE, Lo J, Robertson K. Acute anorectic effect of single and combined drugs in mice using a non-deprivation protocol. Psychopharmacology (Berl). 2001 Sep;157(2):193-6. PubMed PMID: 11594445.
6: Rowland NE, Marshall M, Robertson K. Anorectic effect of dehydroepiandrosterone combined with dexfenfluramine or thionisoxetine. Eur J Pharmacol. 2001 May 4;419(1):61-4. PubMed PMID: 11348631.
7: Rowland NE, Marshall M, Roth JD. Comparison of either norepinephrine-uptake inhibitors or phentermine combined with serotonergic agents on food intake in rats. Psychopharmacology (Berl). 2000 Mar;149(1):77-83. PubMed PMID: 10789886.
8: Gehlert DR, Dreshfield L, Tinsley F, Benvenga MJ, Gleason S, Fuller RW, Wong DT, Hemrick-Luecke SK. The selective norepinephrine reuptake inhibitor, LY368975, reduces food consumption in animal models of feeding. J Pharmacol Exp Ther. 1998 Oct;287(1):122-7. PubMed PMID: 9765330.
9: Gehlert DR, Hemrick-Luecke SK, Schober DA, Krushinski J, Howbert JJ, Robertson DW, Wong DT, Fuller RW. (R)-thionisoxetine, a potent and selective inhibitor of central and peripheral norepinephrine uptake. Life Sci. 1995;56(22):1915-20. PubMed PMID: 7746100.